WO2017147542A3 - Optimized transglutaminase site-specific antibody conjugation - Google Patents

Optimized transglutaminase site-specific antibody conjugation Download PDF

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Publication number
WO2017147542A3
WO2017147542A3 PCT/US2017/019537 US2017019537W WO2017147542A3 WO 2017147542 A3 WO2017147542 A3 WO 2017147542A3 US 2017019537 W US2017019537 W US 2017019537W WO 2017147542 A3 WO2017147542 A3 WO 2017147542A3
Authority
WO
WIPO (PCT)
Prior art keywords
optimized
specific antibody
antibody conjugation
transglutaminase
site
Prior art date
Application number
PCT/US2017/019537
Other languages
French (fr)
Other versions
WO2017147542A2 (en
Inventor
Christopher D'SOUZA
Amy Han
William Olson
Original Assignee
Regeneron Pharmaceuticals, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Regeneron Pharmaceuticals, Inc. filed Critical Regeneron Pharmaceuticals, Inc.
Priority to US16/079,851 priority Critical patent/US11786603B2/en
Priority to EP17711392.5A priority patent/EP3419670A2/en
Publication of WO2017147542A2 publication Critical patent/WO2017147542A2/en
Publication of WO2017147542A3 publication Critical patent/WO2017147542A3/en
Priority to US18/454,521 priority patent/US20240131175A1/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6883—Polymer-drug antibody conjugates, e.g. mitomycin-dextran-Ab; DNA-polylysine-antibody complex or conjugate used for therapy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/1072—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biotechnology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

Provided herein are methods and compositions for site-specific conjugation of antibodies in the presence of a transglutaminase.
PCT/US2017/019537 2016-02-26 2017-02-24 Optimized transglutaminase site-specific antibody conjugation WO2017147542A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
US16/079,851 US11786603B2 (en) 2016-02-26 2017-02-24 Optimized transglutaminase site-specific antibody conjugation
EP17711392.5A EP3419670A2 (en) 2016-02-26 2017-02-24 Optimized transglutaminase site-specific antibody conjugation
US18/454,521 US20240131175A1 (en) 2016-02-26 2023-08-23 Optimized transglutaminase site-specific antibody conjugation

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662300727P 2016-02-26 2016-02-26
US62/300,727 2016-02-26

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US16/079,851 A-371-Of-International US11786603B2 (en) 2016-02-26 2017-02-24 Optimized transglutaminase site-specific antibody conjugation
US18/454,521 Continuation US20240131175A1 (en) 2016-02-26 2023-08-23 Optimized transglutaminase site-specific antibody conjugation

Publications (2)

Publication Number Publication Date
WO2017147542A2 WO2017147542A2 (en) 2017-08-31
WO2017147542A3 true WO2017147542A3 (en) 2017-10-12

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2017/019537 WO2017147542A2 (en) 2016-02-26 2017-02-24 Optimized transglutaminase site-specific antibody conjugation

Country Status (3)

Country Link
US (2) US11786603B2 (en)
EP (1) EP3419670A2 (en)
WO (1) WO2017147542A2 (en)

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CN110944718A (en) 2017-05-18 2020-03-31 里珍纳龙药品有限公司 Cyclodextrin protein drug conjugates
EA201900562A1 (en) 2017-05-18 2020-05-12 Регенерон Фармасьютикалз, Инк. BIS-OCTAGHYDROPHENANTHRENE CARBOXAMIDES AND THEIR PROTEIN CONJUGATES
CA3086926A1 (en) 2018-01-08 2019-07-11 Regeneron Pharmaceuticals, Inc. Steroids and antibody-conjugates thereof
BR112020022400A2 (en) 2018-05-09 2021-02-02 Regeneron Pharmaceuticals, Inc. anti-msr1 antibodies and methods of using them
EA202191430A1 (en) 2018-11-20 2021-11-29 Регенерон Фармасьютикалз, Инк. BIS-OCTAHYDROPHENANTHENETRENE CARBOXAMIDE DERIVATIVES AND THEIR PROTEIN CONJUGATES
KR20210107752A (en) 2018-12-21 2021-09-01 리제너론 파마슈티칼스 인코포레이티드 Rifamycin analogs and antibody-drug conjugates thereof
WO2021211984A1 (en) 2020-04-16 2021-10-21 Regeneron Pharmaceuticals, Inc. Diels-alder conjugation methods
EP4171653A2 (en) * 2020-06-24 2023-05-03 Regeneron Pharmaceuticals, Inc. Tubulysins and protein-tubulysin conjugates
EP4178625A1 (en) 2020-07-13 2023-05-17 Regeneron Pharmaceuticals, Inc. Camptothecin analogs conjugated to a glutamine residue in a protein, and their use
MX2023002974A (en) 2020-09-14 2023-05-25 Regeneron Pharma Antibody-drug conjugates comprising glp1 peptidomimetics and uses thereof.
CA3190569A1 (en) 2020-10-22 2022-04-28 Christopher Daly Anti-fgfr2 antibodies and methods of use thereof
CN117279664A (en) 2021-04-10 2023-12-22 普方生物制药美国公司 FOLR1 binding agents, conjugates thereof, and methods of use thereof
EP4326768A1 (en) 2021-04-23 2024-02-28 Profoundbio Us Co. Anti-cd70 antibodies, conjugates thereof and methods of using the same
CA3238167A1 (en) 2021-11-19 2023-05-25 Maria Leia Smith Gpc3 binding agents, conjugates thereof and methods of using the same
US20230287138A1 (en) 2022-01-12 2023-09-14 Regneron Pharmaceuticals, Inc. Protein-drug conjugates comprising camptothecin analogs and methods of use thereof
WO2023173132A1 (en) 2022-03-11 2023-09-14 Regeneron Pharmaceuticals, Inc. Anti-glp1r antibody-drug conjugates comprising glp1 peptidomimetics and uses thereof

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Also Published As

Publication number Publication date
US11786603B2 (en) 2023-10-17
WO2017147542A2 (en) 2017-08-31
EP3419670A2 (en) 2019-01-02
US20190070306A1 (en) 2019-03-07
US20240131175A1 (en) 2024-04-25

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